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1. 发明授权

US4900839A precursors to Quinolone inotropic agents 失效
标题翻译：喹诺酮变力剂的前体
公开(公告)号：US4900839A
公开(公告)日：1990-02-13
申请号：US302698
申请日：1989-01-27
申请人： Simon F. Campbell , David A. Roberts
发明人： Simon F. Campbell , David A. Roberts
IPC分类号： C07D231/12 , C07D233/61 , C07D257/04 , C07D401/04 , C07D521/00
CPC分类号： C07D257/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04
摘要： A series of novel heterocyclic-substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterocyclic ring moiety is a pyrrolyl, imidazolyl, pyrazolyl, triazolyl or tetrazolyl group attached by a nitrogen atom of said group to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent inotropic agents and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 6-(2,4-dimethylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 6-(2,4-dimethyl-5-nitroimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 8-methyl-6-(tetrazol-1-yl)-2-(1H)-quinolone, 8-methyl-6-(1,2,4-triazol-4-yl)-2-(1H)-quinolone, and 6-(4-cyano-2-methylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, respectively. Methods for preparing these compounds from known starting materials are provided.

2. 发明授权

US4728654A Quinolone inotropic agents 失效
标题翻译：喹诺酮变力剂
公开(公告)号：US4728654A
公开(公告)日：1988-03-01
申请号：US822575
申请日：1986-01-27
申请人： Simon F. Campbell , David A. Roberts
发明人： Simon F. Campbell , David A. Roberts
IPC分类号： C07D401/10 , A61K31/47 , A61K31/495 , A61K31/535 , A61P9/04 , C07D215/18 , C07D215/22 , C07D215/227 , C07D401/12 , C07D521/00 , C07D215/06
CPC分类号： C07D215/227 , C07D215/18 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12
摘要： A series of novel phenyl-substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the phenyl ring moiety is a mono-or di-substituted phenyl group attached to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent inotropic agents and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 8-methyl-6-[4-methylsulphinylphenyl]-2-(1H)-quinolone, 8-methyl-6-[4-hydroxyphenyl]-2-(1H)-quinolone and 8-methyl-6-[4-carbamoylphenyl]-2-(1H)-quinolone, respectively. Methods for preparing these compounds from known starting materials are provided.
摘要翻译：已经制备了一系列新的苯基取代的2-（1H） - 喹诺酮化合物，包括其3,4-二氢衍生物，其中苯环部分是连接到5-，喹诺酮环的6-，7-或8-位。这些特定化合物在治疗中可用作高效力的肌力药物，因此在治疗各种心脏病症中是有价值的。优选的成员化合物包括8-甲基-6- [4-甲基亚磺酰基苯基] -2-（1H） - 喹诺酮，8-甲基-6- [4-羟基苯基] -2-（1H） - 喹诺酮和8-甲基-6- [4-氨基甲酰基苯基] -2-（1H） - 喹诺酮。提供了从已知原料制备这些化合物的方法。

3. 发明授权

US4728653A 6-heteroaryl quinolone inotropic agents 失效
标题翻译： 6-杂芳基喹诺酮变力剂
公开(公告)号：US4728653A
公开(公告)日：1988-03-01
申请号：US844448
申请日：1986-03-26
申请人： Simon F. Campbell , David A. Roberts
发明人： Simon F. Campbell , David A. Roberts
IPC分类号： C07D231/12 , C07D233/61 , C07D257/04 , C07D401/04 , C07D521/00 , A61K31/47
CPC分类号： C07D257/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04
摘要： A series of novel heterocyclic-substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterocyclic ring moiety is a pyrrolyl, imidazolyl, pyrazolyl, triazolyl or tetrazolyl group attached by a nitrogen atom of said group to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent inotropic agents and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 6-(2,4-dimethylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 6-(2,4-dimethyl-5-nitroimadazol-1-yl)-8-methyl-2-(1H)-quinolone, 8-methyl-6-(tetrazol-1-yl)-2-(1H)-quinolone, 8-methyl-6-(1,2,4-triazol-4-yl)-2-(1H)-quinolone, and 6-(4-cyano-2-methylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, respectively. Methods for preparing these compounds from known starting materials are provided.
摘要翻译：已经制备了一系列新的杂环取代的2-（1H） - 喹诺酮化合物，包括其3,4-二氢衍生物，其中杂环部分是通过氮连接的吡咯基，咪唑基，吡唑基，三唑基或四唑基所述基团的原子与喹诺酮环的5-，6-，7-或8-位。这些特定化合物在治疗中可用作高效力的肌力药物，因此在治疗各种心脏病症中是有价值的。优选的成员化合物包括6-（2,4-二甲基咪唑-1-基）-8-甲基-2-（1H） - 喹诺酮，6-（2,4-二甲基-5-硝基咪唑-1-基）-8- （1H） - 喹诺酮，8-甲基-6-（四唑-1-基）-2-（1H） - 喹诺酮，8-甲基-6-（1,2,4-三唑-4-基））-2-（1H） - 喹诺酮和6-（4-氰基-2-甲基咪唑-1-基）-8-甲基-2-（1H） - 喹诺酮。提供了从已知原料制备这些化合物的方法。

4. 发明授权

US4898872A Imidazo[4,5-b]pyridyl quinolone cardiac stimulants 失效
标题翻译：咪唑并[4,5-b]吡啶基喹诺酮心脏兴奋剂
公开(公告)号：US4898872A
公开(公告)日：1990-02-06
申请号：US184462
申请日：1988-04-21
申请人： Simon F. Campbell , David S. Morris , David A. Roberts
发明人： Simon F. Campbell , David S. Morris , David A. Roberts
IPC分类号： C07D215/22 , A61K31/47 , A61K31/50 , A61P9/00 , C07D215/227 , C07D401/04 , C07D471/04
CPC分类号： C07D215/227 , C07D401/04 , C07D471/04
摘要： A series of novel heterobicyclic substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterobicyclic ring moiety is an optionally-substituted indolyl, phthalizinyl, benzimidazolyl, imidazopyridinyl, quinolinyl or isoquinolinyl group attached by an nitrogen or carbon atom of said group to the 6-position of the quinolone ring. The optional substituent is a C.sub.1 -C.sub.14 alkyl group located on either of the two heterobicyclic rings and/or an oxo group situated on the heterocyclic portion of said heterobicyclic ring system. These particular compounds are useful in therapy as cardiac stimulants and therefore, are of value in the treatment of various cardiac conditions. 6-{1(H)-Imidazo[4,5-b]pyridin-6-yl}-8-methyl-2-(1H)-quinolone represents a typical and preferred member compound. Methods for preparing these compounds from known starting materials are provided.

5. 发明授权

US4740513A Methyl substituted imidazol-1-yl quinolones 失效
标题翻译：甲基取代的咪唑-1-基喹诺酮类
公开(公告)号：US4740513A
公开(公告)日：1988-04-26
申请号：US929456
申请日：1986-11-12
申请人： Simon F. Campbell , David A. Roberts
发明人： Simon F. Campbell , David A. Roberts
IPC分类号： C07D401/02 , A61K31/47 , A61K31/4704 , A61P9/04 , C07D233/61 , C07D401/04 , C07D401/14
CPC分类号： C07D401/04 , C07D401/14
摘要： A series of novel heterocyclic-substituted 2-(1H)-quinolone compounds have been prepared wherein the heterocyclic ring moiety is a substituted pyrrolyl, imidazolyl, pyrazolyl, triazolyl or tetrazolyl group attached by a nitrogen atom of said group to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent cardiac stimulants and therefore, are of value in the treatment of various cardiac conditions. Typical member compounds include those 6-(heterocyclic-substituted)-8-methyl-2-(1H)-quinolones wherein the heterocyclic ring moiety is a ring-substituted imidazol-1-yl group and preferably, an imidazol-1-yl group substituted with one or two methyl groups and a monoacetyl group. 6-(4-Acetyl-2-methylimidazol-1-yl)-8-methyl--2-(1H)-quinolone represents a typical and preferred member compound. Methods for preparing all these compounds from known starting materials are provided.
摘要翻译：已经制备了一系列新的杂环取代的2-（1H） - 喹诺酮化合物，其中杂环部分是被所述基团的氮原子连接到5-，6位上的取代的吡咯基，咪唑基，吡唑基，三唑基或四唑基 - ，喹诺酮环的7-或8-位。这些特定化合物在治疗中可用作高效的心脏兴奋剂，因此在治疗各种心脏病症中是有价值的。典型的成员化合物包括那些6-（杂环取代的）-8-甲基-2-（1H） - 喹诺酮，其中杂环部分是环取代的咪唑-1-基，优选咪唑-1-基被一个或两个甲基和单乙酰基取代。 6-（4-乙酰基-2-甲基咪唑-1-基）-8-甲基-2-（1H） - 喹诺酮代表典型和优选的成员化合物。提供了从已知原料制备所有这些化合物的方法。

6. 发明授权

US4542132A Cardiac stimulating cyclic sulfonamido substituted 4-piperidino-quinazoline derivatives, compositions, and method of use therefor 失效
标题翻译：心脏刺激性环亚磺酰氨基取代的4-哌啶子基 - 喹唑啉衍生物，组合物及其使用方法
公开(公告)号：US4542132A
公开(公告)日：1985-09-17
申请号：US636197
申请日：1984-07-31
申请人： Simon F. Campbell , Albert A. Jaxa-Chamiec , David A. Roberts
发明人： Simon F. Campbell , Albert A. Jaxa-Chamiec , David A. Roberts
IPC分类号： C12N9/99 , A61K31/505 , A61K31/54 , A61P9/04 , A61P9/08 , A61P9/10 , A61P43/00 , C07D211/22 , C07D211/32 , C07D211/42 , C07D211/70 , C07D213/30 , C07D401/04 , C07D405/04 , C07D405/14 , C07D417/06 , C07D417/14 , C07F7/18 , A61K31/445
CPC分类号： C07D213/30 , C07D211/42 , C07D211/70 , C07D401/04 , C07D405/04 , C07D405/14 , C07D417/06 , C07D417/14 , C07F7/1856
摘要： A series of novel 4-piperidino-6,7-dimethoxyquinazoline compounds, further substituted on the piperidino group, and the pharmaceutically-acceptable salts thereof, possess cardiac stimulating activity in mammals. They are useful in the curative or prophylactic treatment of cardiac conditions, in particular heart failure.
摘要翻译：在哌啶子基上进一步取代的一系列新的4-哌啶子基-6,7-二甲基喹唑啉化合物及其药学上可接受的盐在哺乳动物中具有心脏刺激活性。它们可用于治疗或预防性治疗心脏病症，特别是心力衰竭。

7. 发明授权

US4837334A Precursors to quinolone inotropic agents 失效
标题翻译：喹诺酮变力剂前体
公开(公告)号：US4837334A
公开(公告)日：1989-06-06
申请号：US125037
申请日：1987-11-23
申请人： Simon F. Campbell , David A. Roberts
发明人： Simon F. Campbell , David A. Roberts
IPC分类号： C07D231/12 , C07D233/61 , C07D257/04 , C07D401/04 , C07D521/00
CPC分类号： C07D257/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04
摘要： A series of novel heterocyclic-substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterocyclic ring moiety is a pyrrolyl, imidazolyl, pyrazolyl, triazolyl or tetrazolyl group attached by a nitrogen atom of said group to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent inotropic agents and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 6-(2,4-dimethylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 6-(2,4-dimethyl-5-nitroimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 8-methyl-6-(tetrazol-1-yl)-2-(1H)-quinolone, 8-methyl-6-(1,2,4-triazol-4-yl)-2-(1H)-quinolone, and 6-(4-cyano-2-methylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, respectively. Methods for preparing these compounds from known starting material are provided.

8. 发明授权

US4783467A Tetrahydroimidazoquinazolinone inotropic agents 失效
标题翻译：四氢咪唑并喹唑啉酮变性剂
公开(公告)号：US4783467A
公开(公告)日：1988-11-08
申请号：US865693
申请日：1986-05-22
申请人： Simon F. Campbell , David A. Roberts
发明人： Simon F. Campbell , David A. Roberts
IPC分类号： C07D487/14 , C07D213/64 , C07D249/08 , C07D487/04 , C07D521/00 , A61K31/505
CPC分类号： C07D213/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D487/04
摘要： A series of novel heterocyclic-substituted 1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-one compounds have been prepared, including their pharmaceutically acceptable salts, wherein the heterocyclic ring moiety is an optionally substituted 5- or 6-membered aromatic heterocyclic group attached to the 6-, 7-, 8- or 9-positions of the aforesaid tetrahydroquinaxolinone ring. These particular compounds are useful in therapy as highly potent inotropic and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 7-(2,4-dimethylimidaxol-1-yl)-9-methyl-1,2,4,5,-tetrahydroimidazo (2,1-b)quinazolin-2-(1H)-one, 3,9-dimethyl-7-(2,4-dimethylimidazol-1-yl) -1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-one and 9-methyl-7 -(1,2,4-triazol-4-yl)-1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-one, respectively. Methods for preparing these compounds from known starting materials are provided.
摘要翻译：已经制备了一系列新的杂环取代的1,2,3,5-四氢咪唑并（2,1-b）喹唑啉-2-（1H） - 酮化合物，包括其药学上可接受的盐，其中杂环部分是任选取代的与上述四氢喹啉酮环的6-，7-，8-或9-位连接的5元或6元芳族杂环基。这些特定化合物在治疗中可用作高度有效的肌力，因此在各种心脏病症的治疗中具有价值。优选的成员化合物包括7-（2,4-二甲基咪唑烷-1-基）-9-甲基-1,2,4,5， - 四氢咪唑并（2,1-b）喹唑啉-2-（1H） - 酮，3 ，9-二甲基-7-（2,4-二甲基咪唑-1-基）-1,2,3,5-四氢咪唑并（2,1-b）喹唑啉-2-（1H） - 酮和9-甲基-7 - （1,2,4-三唑-4-基）-1,2,3,5-四氢咪唑并（2,1-b）喹唑啉-2-（1H） - 酮。提供了从已知原料制备这些化合物的方法。

9. 发明授权

US4710507A Quinolone inotropic agents 失效
标题翻译：喹诺酮变力剂
公开(公告)号：US4710507A
公开(公告)日：1987-12-01
申请号：US683440
申请日：1984-12-18
申请人： Simon F. Campbell , David A. Roberts
发明人： Simon F. Campbell , David A. Roberts
IPC分类号： C07D401/14 , A61K31/4704 , A61P9/04 , C07D213/40 , C07D215/18 , C07D215/22 , C07D215/227 , C07D215/28 , C07D215/48 , C07D215/54 , C07D401/04 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , A61K31/47
CPC分类号： C07D213/40 , C07D215/18 , C07D215/227 , C07D215/28 , C07D215/48 , C07D215/54 , C07D401/04 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： A heterocyclic-substituted 2-quinolone compound of the formula: ##STR1## or a pharmaceutically-acceptable salt thereof, wherein "Het" is an optionally substituted 5-or 6-membered monocyclid aromatic heterocyclic group attached by a carbon atom to the 5-, 6-, 7- or 8- position of the quinolone nucleus; R, which is attached to the 5-, 6-, 7- or 8- position, is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphinyl, C.sub.1 -C.sub.4 alkylsulphonyl, halo, CF.sub.3, hydroxy, hydroxymethyl, or cyano; R.sup.1 is hydrogen, cyano (C.sub.1 -C.sub.4 alkoxy)carbonyl, C.sub.1 -C.sub.4 alkyl, nitro, halo, --NR.sup.3 R.sup.4 or --CONR.sup.3 R.sup.4 where each of R.sup.3 and R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic group optionally containing a further heteroatom or group selected from O, S and N--R.sup.5 where R.sup.5 is hydrogen or C.sub. 1 -C.sub.4 alkyl; R.sup.2 is hydrogen, C.sub.1 -C.sub.4 alkyl, or 2-hydroxyethyl; Y is hydrogen or C.sub.1 -C.sub.4 alkyl; and the dotted line between the 3- and 4- positions represents an optional bond. The compounds are inotropic agents useful as cardiac stimulants in the treatment of congestive heart failure.
摘要翻译：式（I）的杂环取代的2-喹诺酮化合物或其药学上可接受的盐，其中“Het”是通过碳原子连接的任选取代的5元或6元单环芳族杂环基，喹诺酮核的5-，6-，7-或8-位; 连接在5-，6-，7-或8-位的R是氢，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4烷基亚磺酰基，C 1 -C 4烷基磺酰基，卤素， CF 3，羟基，羟甲基或氰基; R 1是氢，氰基（C 1 -C 4烷氧基）羰基，C 1 -C 4烷基，硝基，卤素，-NR 3 R 4或-CONR 3 R 4，其中R 3和R 4各自是氢或C 1 -C 4烷基或R 3和R 4与氮原子一起它们连接形成饱和的5-或6-元杂环基团，任选地含有另外的杂原子或选自O，S和N-R5的基团，其中R 5是氢或C 1 -C 4烷基; R2是氢，C1-C4烷基或2-羟基乙基; Y是氢或C 1 -C 4烷基; 3-和4-位之间的虚线表示任选的键。这些化合物是用于治疗充血性心力衰竭的心脏兴奋剂的变力剂。

10. 发明授权

US4489075A Cyclic sulfonamidoalkyl substituted 4-piperidinoquinazoline cardiac stimulants 失效
标题翻译：环亚磺酰氨基烷基取代的4-哌啶子基喹唑啉心脏兴奋剂
公开(公告)号：US4489075A
公开(公告)日：1984-12-18
申请号：US489271
申请日：1983-04-27
申请人： Simon F. Campbell , David A. Roberts , John K. Stubbs
发明人： Simon F. Campbell , David A. Roberts , John K. Stubbs
IPC分类号： A61K31/517 , A61K31/4523 , A61K31/505 , A61K31/54 , A61P9/04 , A61P43/00 , C07D211/22 , C07D211/26 , C07D213/30 , C07D213/38 , C07D239/94 , C07D285/16 , C07D401/04 , C07D417/06 , C07D417/14 , A61K31/445
CPC分类号： C07D213/30 , C07D211/22 , C07D213/38 , C07D285/16 , C07D401/04 , C07D417/06 , C07D417/14
摘要： 6,7-Dialkoxy-4-[4-(cyclic-sulfonamidoalkyl)piperidino]quinazolines and method of use as cardiac stimulants.
摘要翻译： 6,7-二烷氧基-4- [4-（环亚磺酰氨基烷基）哌啶子基]喹唑啉和用作心脏兴奋剂的方法。

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